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mitozolomide

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Description

mitozolomide: RN & structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71766
CHEMBL ID435951
SCHEMBL ID97695
MeSH IDM0120254

Synonyms (49)

Synonym
{imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide,} 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
3-(2-chloroethyl)-4-oxo-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
3-(2-chloroethyl)-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetraazine-8-carboxamide
NCI60_003169
ccrg-81080
46241-rp
m&b-39565
8-carbamoyl-3-(2-chloroethyl)imidazo(5,1-d)-1,2,3,5-tetrazin-4(3h)-one
3-(2-chloroethyl)-3,4-dihydro-4-oxoimidazo(5,1-d)-as-tetrazine-8-carboxamide
3-(2-chloroethyl)-3,4-dihydro-4-oxoimidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide
m & b 39565
einecs 287-943-3
mitozolamide
mitozolomida [spanish]
brn 3618072
ccrg 81010
imidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide, 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
nsc 353451
mitozolomidum [latin]
mitozolomide
nsc-353451
imidazo[5,2,3,5-tetrazine-8-carboxamide, 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
azolastone
85622-95-3
mls003171125 ,
nsc353451
CHEMBL435951
3-(2-chloroethyl)-4-oxoimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
smr001875033
mitozolomide [inn:ban]
e3u7286v3w ,
mitozolomida
unii-e3u7286v3w
mitozolomidum
FT-0630937
mitozolomide [inn]
SCHEMBL97695
DTXSID40234862
3-(2-chloroethyl)-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetraazine-8-carboxamide #
QXYYYPFGTSJXNS-UHFFFAOYSA-N
imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide, 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
3-(2-chloroethyl)-3,4-dihydro-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide
8-carbamoyl-3-(2-chloroethyl)-imidazo[5,1-d]-1,2,3,5-tetrazin-4-one
8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3h)-one
Q6881926
3-(2-chloroethyl)-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
3-(2-chloroethyl)-4-oxo-3h,4h-imidazo[4,3-d][1,2,3,5]tetrazine-8-carboxamide
EN300-23093670
Z2044764896

Research Excerpts

Overview

Mitozolomide is a novel antitumour agent showing a broad spectrum of activity against murine tumours. It is currently undergoing Phase I clinical evaluation in the UK.

ExcerptReferenceRelevance
"Mitozolomide is a novel antitumour agent showing a broad spectrum of activity against murine tumours and is currently undergoing Phase I clinical evaluation in the UK. "( Antitumour imidazotetrazines, Part IX. The pharmacokinetics of mitozolomide in mice.
Goddard, C; Slack, JA; Stevens, MF, 1985
)
1.95

Toxicity

ExcerptReferenceRelevance
" In comparison with control cells that were transfected with the parent vector, the ATase-expressing clones were considerably more resistant to the toxic effects of the methylating agents N-methyl-N-nitrosourea and methylmethanesulphonate or the chloroethylating agents Mz or taurine chloroethylnitrosourea, but unchanged in their susceptibility to the bis-chloroethylating agent nitrogen mustard."( Transfection of murine multi-potent haemopoietic stem cells with an E. coli DNA alkyltransferase gene confers resistance to the toxic effects of alkylating agents.
Dexter, TM; Jelinek, J; Kleibl, K; Margison, GP, 1988
)
0.27
" M&B 39565 and MCTIC were 5- to 6-fold more toxic to VA-13 cells than to IMR-90 cells for drug concentrations which produced a 2-log cell kill, as measured by colony-forming assays."( DNA cross-linking and cytotoxicity in normal and transformed human cells treated in vitro with 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d] -1,2,3,5-tetrazin-4(3H)-one.
Erickson, LC; Gibson, NW; Hickman, JA, 1984
)
0.27
"001) to the toxic effects of this drug."( Recombinant adeno-associated virus-mediated expression of O6-alkylguanine-DNA-alkyltransferase protects human epithelial and hematopoietic cells against chloroethylating agent toxicity.
Arrand, JR; Berns, KI; Cortez, N; Fairbairn, LJ; Giraud, C; Longhurst, SJ; Rafferty, JA, 1999
)
0.3

Pharmacokinetics

ExcerptReferenceRelevance
" In an attempt to relate dose and pharmacokinetic parameters to toxicity, we measured plasma concentrations of mitozolomide in 14 patients with a range of malignancies."( Relationship between the pharmacokinetics and toxicity of mitozolomide.
Blackledge, GR; Bradley, C; Kaye, SB; Kerr, DJ; Secrett, P; Slack, JA; Stevens, MF, 1990
)
0.73
" We have conducted an animal pharmacokinetic study using male BALB/c mice as a pre-requisite to the clinical work."( Antitumour imidazotetrazines, Part IX. The pharmacokinetics of mitozolomide in mice.
Goddard, C; Slack, JA; Stevens, MF, 1985
)
0.51

Dosage Studied

ExcerptRelevanceReference
" The major toxicity was myelosuppression which necessitated reduction in the initial dosage from 115 to 90 mg/m2."( Phase II studies of mitozolomide in melanoma, lung and ovarian cancer.
Docherty, V; Dorward, A; Harding, M; Kaye, S; Mackie, R, 1989
)
0.6
" MTZ, according to this schedule and dosage does not show significant activity in human squamous cell head and neck cancer."( Phase II study of mitozolomide (M & B 39,565) in head and neck cancer.
Armand, JP; Benahmed, M; Cvitkovic, E; Delgado, FM; Domenge, C; Fontana, X; Herait, P; Recondo, G, 1989
)
0.61
"8%, respectively, of those seen when mice were dosed with authentic methylmitozolomide."( Metabolism and murine pharmacokinetics of the 8-(N,N-dimethylcarboxamide) analogue of the experimental antitumor drug mitozolomide (NSC353451).
Gescher, A; Horspool, KR; Lunt, E; Quarterman, CP; Slack, JA; Stevens, MF, 1989
)
0.72
" Since high levels of the enzyme confer the efficient repair of DNA alkylation, the chemotherapeutic potential of alkylating chemicals can be maintained either increasing drug dosage or reducing the amount of endogenous MGMT."( The sensitivity of MCF10A breast epithelial cells to alkylating drugs is enhanced by the inhibition of O6-methylguanine-DNA methyltransferase transcription with a synthetic double strand DNA oligonucleotide.
Citti, L; Colombo, MG; Mariani, L; Piccirilli, A; Poliseno, L; Rainaldi, G, 2002
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (174)

Assay IDTitleYearJournalArticle
AID120186Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119622Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119612Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124600Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 -5 T/C = days test animals live/days control animals live x 100; >60/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100953Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and number of Survivors to duration was reported at 40 mg/kg peroral dose; 1/71987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID120170Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on days 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122064Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120169Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16927Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID120177Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24905Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Centigrade in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID712167Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin22012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID100972Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 20 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID122067Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120181Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24901Half life for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID81318In vitro cytotoxicity against human xeroderma pigmentosum fibroblast cells HMGZAT (mer+)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID209692In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 5 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID122066Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124728Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >60/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122046Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119615Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16925Mean rate constant for the hydrolysis of compound in buffers at pH 7.4 at 37 degrees Centigrade in incubation mixture - d(A)-d(T) (10:!)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID712168Cytotoxicity against human A2780 cells after 5 days by MTT assay2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID209551In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 20 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID100946In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 40 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID122063Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122065Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24906Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID16923Mean rate constant for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119608Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122050Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119606Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16928Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119617Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120185Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122047Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122059Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120182Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209544In vitro cytotoxicity against mouse TLX5 lymphoma cells1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119623Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124735Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 15/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID28475Hydrolytic parameter (K) was calculated at pH 7.4 in 0.1 M phosphate buffer (25 degrees Celsius)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID209859Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 5 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID124719Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; 12.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID26695Half-life period in 95% ethanol in dark at 28 degrees celsius.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122051Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120173Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID712166Cytotoxicity against MMR-deficient human A2780/CP70 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin22012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID26697Half-life period in 95% ethanol in diffuse laboratory light at 28 degrees celsius.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120172Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122062Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122068Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124736Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 13.2/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124731Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; >60/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100947In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 5 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID124721Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; 11.3/8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209688In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 20 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID16924Mean rate constant for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID16926Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - 5'-GMP/5'-CMP (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID73184In vitro cytotoxicity against human lymphoblastoid cell line (GM892 A)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID120189Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120180Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124724Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; 15.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119610Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124716Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 16/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122052Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119609Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124727Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 16.4/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122049Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122069Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID766221Ratio of IC50 for human HCT116 cells expressing p53 to IC50 for p53-deficient human HCT116 cells2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA-methyltransferase, DNA mismatch repair, and p53.
AID124601Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 10.6/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119613Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209983In vitro cytotoxicity against mouse TLX5 lymphoma cells2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID124718Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; >61.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119620Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124739Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >60/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119598Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24902Half life for the hydrolysis of compound in buffers at pH 7.4 at 37 degrees Celsius in incubation mixture - d(A)-d(T) (10:!)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID120188Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124726Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 14.1/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120183Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119603Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on days 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100975Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 5 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID24900Half life for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119611Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120165Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124717Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on days 1-5 T/C = days test animals live/days control animals live x 100; >60/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16929Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID122056Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120174Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124715Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 11.6/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124725Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 17.0/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID27023Half life calculated for hydrolysis in 0.1 M phosphate buffer at 37 degrees Centigrade (pH 7.4)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID120179Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119626Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID712165Cytotoxicity against MMR-deficient human A2780/CP70 cells after 5 days by MTT assay2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID100923In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 20 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID209706Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and number of Survivors to duration was reported at 40 mg/kg ip dose; 4/51987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID100944In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 20 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID81319In vitro cytotoxicity against human xeroderma pigmentosum fibroblast cells HMGZip (mer-)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID124714Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >61.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120164Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID27022Half life calculated for hydrolysis in 0.1 M phosphate buffer at 25 degrees Celsius (pH 7.4)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID231797Ratio of cytotoxicity against Raji cells to that of GM892 A cells.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID124732Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >60/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124730Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 16/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122055Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124729Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 27/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119604Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119618Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119601Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120190Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122053Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209548In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 10 mg/kg on 5th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID124734Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; >60/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209690In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 40 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID100969Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 10 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID119600Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122058Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209856Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 40 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID28476Hydrolytic parameter (K) was calculated at pH 7.4 in 0.1 M phosphate buffer (37 degrees Celsius)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID120166Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122070Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16930Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID124738Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 17.8/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209685In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 10 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID24907Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID26698Half-life period in phosphate buffer at pH 7.4 in the dark at 28 degrees celsius.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120168Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100943In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 10 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID24903Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Centigrade in incubation mixture - 5'-GMP/5'-CMP (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119624Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124733Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 38/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122048Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120178Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120175Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID165776In vitro cytotoxicity against Raji cell line1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119605Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122054Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209557In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 5 mg/kg on 5th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID120184Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119619Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119602Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209852Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 20 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID124737Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 30/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID766223Chemosensitization of human HCT116 cells expressing p53 after 5 days by MTT assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA-methyltransferase, DNA mismatch repair, and p53.
AID124720Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; > 60/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100927In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 5 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID119599Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on days 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120171Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122057Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120176Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124722Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 9.0/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120332Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122061Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119616Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124740Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 7.4 / 10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119614Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100973Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 40 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID24904Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119625Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120187Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209847Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 10 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID119607Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119621Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209556In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 40 mg/kg on 5th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID120167Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124723Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 14.4/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100922In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 10 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID100926In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 40 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID122060Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID766222Chemosensitization of p53-deficient human HCT116 cells after 5 days by MTT assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA-methyltransferase, DNA mismatch repair, and p53.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (75)

TimeframeStudies, This Drug (%)All Drugs %
pre-199040 (53.33)18.7374
1990's25 (33.33)18.2507
2000's6 (8.00)29.6817
2010's4 (5.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.05

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.05 (24.57)
Research Supply Index4.41 (2.92)
Research Growth Index4.16 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (3.85%)5.53%
Reviews1 (1.28%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other74 (94.87%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]